New modulated design and synthesis of quercetin–CuII/ZnII–Sn2IV scaffold as anticancer agents: in vitro DNA binding profile, DNA cleavage pathway and Topo-I activity

2013 ◽  
Vol 42 (27) ◽  
pp. 10029 ◽  
Author(s):  
Sartaj Tabassum ◽  
Mehvash Zaki ◽  
Mohd. Afzal ◽  
Farukh Arjmand
Keyword(s):  
Dna Binding ◽  
Anticancer Agents ◽  
Dna Cleavage ◽  
Binding Profile ◽  
Design And Synthesis

scholarly journals Synthesis and Experimental Validation of New Designed Heterocyclic Compounds with Antiproliferative Activity versus Breast Cancer Cell Lines MCF-7 and MDA-MB-231

2017 ◽  
Vol 2017 ◽  
pp. 1-10 ◽  
Author(s):  
Vincenza Barresi ◽  
Carmela Bonaccorso ◽  
Domenico A. Cristaldi ◽  
Maria N. Modica ◽  
Nicolò Musso ◽  
...  
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Cancer Cell Line ◽  
Breast Cancer Cell Lines ◽  
Design And Synthesis ◽  
Human Breast Cell ◽  
Mcf 7

Recent drug discovery efforts are highly focused towards identification, design, and synthesis of small molecules as anticancer agents. With this aim, we recently designed and synthesized novel compounds with high efficacy and specificity for the treatment of breast tumors. Based on the obtained results, we constructed a Volsurf+ (VS+) model using a dataset of 59 compounds able to predict the in vitro antitumor activity against MCF-7 cancer cell line for new derivatives. In the present paper, in order to further verify the robustness of this model, we report the results of the projection of more than 150 known molecules and 9 newly synthesized compounds. We predict their activity versus MCF-7 cell line and experimentally verify the in silico results for some promising chosen molecules in two human breast cell lines, MCF-7 and MDA-MB-231.

New binuclear Ni(ii) metallates containing ONS chelators: synthesis, characterisation, DNA binding, DNA cleavage, protein binding, antioxidant activity, antimicrobial and in vitro cytotoxicity

2017 ◽  
Vol 41 (7) ◽  
pp. 2543-2560 ◽  
Author(s):  
G. Kalaiarasi ◽  
Ruchi Jain ◽  
H. Puschman ◽  
S. Poorna Chandrika ◽  
K. Preethi ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Dna Binding ◽  
Protein Binding ◽  
Hela Cell ◽  
Antiproliferative Activity ◽  
Dna Cleavage ◽  
In Vitro Cytotoxicity ◽  
Hela Cell Lines ◽  
Mcf 7

Four new binuclear nickel(ii) metallates showed promising antiproliferative activity against MCF-7 and HeLa cell lines and were much less toxic against HaCaT.

Design and Synthesis of Some Novel Aromatic Amide Derivatives of Nilutamide as In Vitro Anticancer Agents

2020 ◽  
Vol 5 (39) ◽  
pp. 12317-12319
Author(s):  
Narasimha Swamy Thirukovela ◽  
Satheesh Kumar Nukala ◽  
Narsimha Sirassu ◽  
Ravinder Manchal ◽  
Prasad Gundepaka ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Design And Synthesis ◽  
Amide Derivatives ◽  
Aromatic Amide ◽  
Derivatives Of

Phenanthridine derivatives as promising new anticancer agents: synthesis, biological evaluation and binding studies

2020 ◽  
Vol 12 (8) ◽  
pp. 709-739 ◽  
Author(s):  
Iqbal Azad ◽  
Rumana Ahmad ◽  
Tahmeena Khan ◽  
Mohammad Saquib ◽  
Firoj Hassan ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Dna Cleavage ◽  
High Resolution Mass Spectrometry ◽  
Biological Evaluation ◽  
Binding Studies ◽  
Binding Properties ◽  
One Pot ◽  
Docking Analysis ◽  
Dna Cleavage Activity

Aim: Phenanthridines are an essential class of nitrogenous heterocycles with extensive applications in medicinal chemistry. The development of efficient and eco-friendly methods for the preparation of chirally pure dihydropyrrolo[1,2- f]phenanthridines (5a–h), and their in vitro evaluation and modeling studies as potential anticancer, antioxidant and DNA cleavage agents is reported. Methodology & results: Compounds 5a–h were prepared through a facile one-pot synthesis and characterized by infrared, high resolution mass spectrometry, 1H and 13C nuclear magnetic resonance. The molecules were subjected to virtual screening and docking analysis against selected human molecular targets. Compound 5g displayed good binding properties as well as significant anticancer and DNA cleavage activity. Conclusion: Compound 5g has been identified as a potential lead candidate for further testing against additional cancer cell lines and animal models in future.

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